A Facile Synthesis of Raltegravir Potassium—An HIV Integrase Inhibitor. (14th August 2019)

• Record Type: Journal Article
• Authors: Karumanchi, Kishore; Nangi, Gangadhara Bhima Shankar; Danda, Subba Reddy; Chavakula, Ramadas; Korupolu, Raghu Babu; Bonige, Kishore Babu
• Is Part Of: Journal of heterocyclic chemistry. Volume 56:Number 9(2019)
• Page Start: 2683
• Page End: 2690
• Publication Date: 2019-08-14
• Subjects: Heterocyclic compounds -- Periodicals; 547.59
• DOI: 10.1002/jhet.3663
• Languages: English
• ISSNs: 0022-152X

Abstract

Abstract : A facile, cost‐effective, and commercially viable synthesis of Raltegravir Potassium (1 ) has been developed from 2‐(1‐amino‐1‐methyl‐ethyl)‐ N ‐[(4‐fluorophenyl)methyl]‐1, 6‐dihydro‐5‐hydroxy‐1‐methyl‐6‐oxo‐4‐pyrimidinecarboxamide (9 ) with high purity and in good yields. In addition, a new approach for the synthesis of key amine intermediate (9 ) of Raltegravir Potassium (1 ) from commercially available 2‐amino‐2‐methylpropanenitrile hydrochloride (2 ) is also described. The key features of the synthesis are fewer synthetic steps, employing the inexpensive reagents and eco‐friendly. Abstract :